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Assay Detail

CHEMBL954074

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Functional
Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Aminopyrazine CB1 receptor inverse agonists.
Wustrow DJ, Maynard GD, Yuan J, Zhao H, Mao J, Guo Q, Kershaw M, Hammer J, Brodbeck RM, Near KE, Zhou D, Beers DS, Chenard BL, Krause JE, Hutchison AJ.
Bioorg Med Chem Lett (2008) 18 : 3376 -3381
PubMed 18448340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.17 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111 RIMONABANT 4.0 1 9.51
CHEMBL497557 1 9.39
CHEMBL496091 1 9.08
CHEMBL498783 1 8.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111 RIMONABANT Ki = 0.31 nM 9.51
CHEMBL497557 Ki = 0.41 nM 9.39
CHEMBL496091 Ki = 0.83 nM 9.08
CHEMBL498783 Ki = 2.06 nM 8.69